Solid dispersion as an approach for bioavailability enhancement of poorly water-soluble drug ritonavir

AAPS PharmSciTech

Volumn 11, Issue 2, 2010, Pages 518-527

  Sinha, Shilpi ^a   Ali, Mushir ^b   Baboota, Sanjula ^b   Ahuja, Alka ^b   Kumar, Anil ^b   Ali, Javed ^b  

^a Jubilant Organosys ^*  (India)

^b HAMDARD UNIVERSITY   (India)

Author keywords

Bioavailability; Gelucire; Poorly soluble drug; Ritonavir; Solid dispersion

Indexed keywords

CHLORIDE; DRUG CARRIER; GELUCIRE; RITONAVIR; SOLVENT; WATER; COLLOID; HUMAN IMMUNODEFICIENCY VIRUS PROTEINASE INHIBITOR; TRIACYLGLYCEROL;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; CALORIMETRY; CONTROLLED STUDY; DIFFERENTIAL SCANNING CALORIMETRY; DISSOLUTION; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG ELIMINATION; DRUG SOLUBILITY; ELECTRON MICROSCOPY; EVAPORATION; FEMALE; FOOD; FOURIER TRANSFORM MASS SPECTROMETRY; IN VITRO STUDY; MALE; MAXIMUM PLASMA CONCENTRATION; NONHUMAN; PERFORMANCE; PRIORITY JOURNAL; RAT; SCANNING ELECTRON MICROSCOPY; SEX; WISTAR RAT; X RAY; X RAY DIFFRACTION; ANIMAL; BLOOD; CHEMISTRY; COLLOID; METABOLIC CLEARANCE RATE; ORAL DRUG ADMINISTRATION; SOLUBILITY;

ADMINISTRATION, ORAL; ANIMALS; COLLOIDS; DRUG CARRIERS; FEMALE; HIV PROTEASE INHIBITORS; MALE; METABOLIC CLEARANCE RATE; RATS; RATS, WISTAR; RITONAVIR; SOLUBILITY; TRIGLYCERIDES; WATER;

EID: 77954805866     PISSN: None     EISSN: 15309932     Source Type: Journal    
DOI: 10.1208/s12249-010-9404-1     Document Type: Article

References (16)

1. Lipinski CA, Lombardo F, Dominyl BW, Feeney PJ. Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings. Adv Drug Deliv Rev. 1997;23:3-25. doi:10.1016/S0169-409X (96) 00423-1.
2. Dannenfelser R, He H, Joshi Y, Bateman S, Serajuddin A T M. Development of clinical dosage forms for a poorly water soluble drug I: Application of polyethylene glycol-polysorbate 80 solid dispersion carrier system. J Pharm Sci. 2004;93:1165-75. doi:10.1002/jps.20044. (Pubitemid 38529690)
3. Mooter G V D, Augustijns P, Blaton N, Kinget R. Physico-chemical characterization of solid dispersions of temazepam with polyethylene glycol 6000 and PVP K30. Int J Pharm. 1998;164:67-80. doi:10.1016/S0378-5173 (97) 00401-8.
4. Habib MJ. Pharmaceutical solid dispersion technology. Washington: CRC; 2000. p. 35-78.
5. Law D, Krill SL, Schmitt EA, Fort JJ, Qiu Y, Wang W et al. Physicochemical considerations in the preparation of amorphous ritonavir-poly (ethylene glycol) 8000 solid dispersions. J Pharm Sci. 2000;90:1015-25. doi:10.1002/jps.1054.
6. Pignatello R, Ferro M, Guidi GD, Salemi G, Vandelli MA, Guccione S et al. Preparation, characterisation and photosensitivity studies of solid dispersions of diflunisal and Eudragit RS100 and RL100. Int J Pharm. 2001;218:27-42. doi:10.1016/S0378-5173 (01) 00597-X.
7. Babu G V M, Prasad DS, Murthy K V R. Evaluation of modified gum karaya as carrier for the dissolution enhancement of poorly water-soluble drug Nimodipine. Int J Pharm. 2002;234:1-17. doi:10.1016/S0378-5173 (01) 00925-5.
8. Hancock BC, Zografi G. Characteristics and significance of the amorphous state in pharmaceutical systems. J Pharm Sci. 1997;86:1-12. doi:10.1021/ js9601896.
9. Gowariker VR, Viswanathan NV, Sreedhar J. Polymer science. New Delhi: New Age; 1986. p. 150-79.
10. Serajuddin A T M. Solid dispersion of poorly water-soluble drugs: early promises, subsequent problems, and recent breakthroughs. J Pharm Sci. 1999;88:1058-66. doi:10.1021/js980403l. (Pubitemid 29480600)
11. Barker SA, Yap SP, Yuen KH, McCoy CP, Murphy JR, Craig D Q M. An investigation in to structure and bioavailability of α-tocopherol in Gelucire 44/14. J Control Release. 2003;91:477-88. doi:10.1016/S0168-3659 (03) 00261-X.
12. Nilüfer Y, Aysegül K, Yalçin Ö, Ayhan S, Sibel AÖ, Tamer B. Enhanced bioavailability of piroxicam using Gelucire 44/14 and Labrasol: in vitro and in vivo evaluation. Eur J Pharm Biopharm. 2003;56:453-9. doi:10.1016/S0939-6411 (03) 00142-5.
13. Ozkan Y, Doganay N, Dikmen N, Isimer A. Enhanced release of solid dispersions of etodolac in polyethylene glycol. Farmaco. 2000;55:433-8.
14. Damian F, Blaton N, Naesens L, Balzarini J, Kinget R, Augustijns P et al. Physicochemical characterization of solid dispersions of the antiviral agent UC-781 with polyethylene glycol 6000 and Gelucire 44/14. Eur J Pharm Sci. 2000;10:311-22. doi:10.1016/S0928-0987 (00) 00084-1.
15. Kanaze FI, Kokkalou E, Niopas I, Georgarakis M, Stergiou A, Bikiaris D. Novel drug delivery systems for flavonoid compounds with enhanced solubility based on solid dispersions with polyvinylpyrolidone and polyethyleneglycol. J Appl Polym Sci. 2006;102:460-71. doi:10.1002/app. 24200.
16. Sekar V, Kestens D, Spinosa-Guzman S. The effect of different meal types on the pharmacokinetics of Darunavir (TMC114)/Ritonavir in HIV-Negative Healthy Volunteers. J Clin Pharmacol. 2007;47:479-84.